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31. 发明授权

US4084002A Pharmaceutical compositions containing a 1-phenoxy-2-hydroxy-3-alkynylamino-propane and method of use 失效
公开(公告)号：US4084002A
公开(公告)日：1978-04-11
申请号：US742639
申请日：1976-11-17
申请人： Herbert Koppe , Werner Kummer , Helmut Stahle , Gojko Muacevic
发明人： Herbert Koppe , Werner Kummer , Helmut Stahle , Gojko Muacevic
IPC分类号： C07C275/34 , A61K31/135
CPC分类号： C07C275/34
摘要： Pharmaceutical dosage unit compositions containing as an active ingredient a 1-aryloxy-2-hydroxy-3-alkynylamino-propane selected from the group consisting of racemic or optically active compounds of the formula ##STR1## wherein R.sub.1 is a member selected from the group consisting of hydrogen; halogen; nitro; alkyl having from 1 to 5 carbon atoms; alkoxy having from 1 to 4 carbon atoms; alkenyl having from 2 to 5 carbon atoms; alkynyl having from 2 to 5 carbon atoms; alkylamino having from 1 to 5 carbon atoms; dialkylamino having from 1 to 5 carbon atoms in each alkyl; alkoxyalkyl having from 2 to 6 carbon atoms; alkylaminoalkyl having from 2 to 6 carbon atoms; dialkylaminoalkyl having from 3 to 12 carbon atoms; --(CH.sub.2).sub.x -NH.sub.2 or --(CH.sub.2).sub.x -OH, where x is an integer from 0 to 3; alkynyloxy having from 3 to 6 carbon atoms; alkenyloxy having from 3 to 6 carbon atoms; --CO-R.sub.9, where R.sub.9 is a member selected from the group consisting of alkyl having 1 to 6 carbon atoms, phenylalkyl having 7 to 10 carbon atoms and phenyl; cycloalkyl having from 3 to 7 carbon atoms; phenyl; phenyl substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and nitro; phenoxy; and phenoxy substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy and nitro;R.sub.2 is a member selected from the group consisting of hydrogen, halogen, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms, alkanoyl having from 2 to 4 carbon atoms, alkenyl having from 2 to 4 carbon atoms, amino and nitro;R.sub.3 is a member selected from the group consisting of hydrogen, halogen, alkyl having from 1 to 4 carbon atoms, alkoxy having from 1 to 4 carbon atoms and, together with R.sub.2 in the ortho-position, --CH.dbd.CH-CH.dbd.CH- or --(CH.sub.2).sub.n --, where n is an integer from 3 to 5;R.sub.4 is a member selected from the group consisting of hydrogen and alkyl having from 1 to 3 carbon atoms; andR.sub.5 is a member selected from the group consisting of alkyl having from 1 to 3 carbon atoms, and, together with R.sub.4, --(CH.sub.2).sub.p --, where p is an integer from 4 to 6;And physiologically compatible acid addition salts thereof; and a method of using the same as adrenolytics and hypotensives.

32. 发明授权

US4025646A Pharmaceutical compositions containing a 1-(cyano-phenoxy)-2-hydroxy-3-hydroxyalkylamino-propane and method of use 失效
标题翻译：含有1-（氰基 - 苯氧基）-2-羟基-3-羟基烷基氨基丙烷的药物组合物及其使用方法
公开(公告)号：US4025646A
公开(公告)日：1977-05-24
申请号：US652113
申请日：1976-01-26
申请人： Herbert Koppe , Helmut Stahle , Werner Kummer , Werner Traunecker
发明人： Herbert Koppe , Helmut Stahle , Werner Kummer , Werner Traunecker
IPC分类号： C07D317/64 , A61K31/275
CPC分类号： C07D317/64
摘要： Pharmaceutical compositions containing as an active ingredient a racemic or optically active compound of the formula ##STR1## wherein R.sub.1 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms, andR.sub.2 is straight or branched hydroxyalkyl of 3 to 6 carbon atoms,Or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as .beta.-adrenergic receptor blocking agents and hypotensives.
摘要翻译：含有下式的外消旋或旋光活性化合物作为活性成分的药物组合物，其中R 1是氢，卤素，1至4个碳原子的烷基或1至4个碳原子的烷氧基，R 2是直链或支链羟烷基 3至6个碳原子，或非毒性，药理学上可接受的酸添加盐; 以及将其用作β-受体阻断剂阻断剂和高血压药物的方法。

33. 发明授权

US3998956A Pharmaceutical compositions containing a 1-(thienyl-methyl)-2-anilino-2-imidazoline and method of use 失效
标题翻译：含有1-（噻吩基 - 甲基）-2-苯胺基-2-咪唑啉的药物组合物及其使用方法
公开(公告)号：US3998956A
公开(公告)日：1976-12-21
申请号：US639341
申请日：1975-12-10
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Klaus Stockhaus
IPC分类号： A61K31/415 , G03G15/08
CPC分类号： A61K31/415 , G03G15/08
摘要： Pharmaceutical compositions containing as an active ingredient a compound of the formula ##STR1## wherein R, R.sub.1 and R.sub.2 are each hydrogen, fluorine, chlorine, bromine, methyl, ethyl, methoxy, trifluoromethyl or cyano, andR.sub.5 is hydrogen, methyl or ethyl, or a non-toxic, pharmaceutically acceptable acid addition salt thereof; and a method of using the same as analgesics and hypotensives.
摘要翻译：其中R 1，R 2和R 2各自为氢，氟，氯，溴，甲基，乙基，甲氧基，三氟甲基或氰基，R 5为氢，甲基或乙基，或其无毒的药学上可接受的酸加成盐; 以及使用它们作为镇痛药和低血压药物的方法。

34. 发明授权

US3969512A N,N'bis-(3-phenoxy-2-hydroxy-propyl)-alkylenediamines and salts thereof 失效
标题翻译： N，N（40-双（3-苯氧基-2-羟基 - 丙基） - 亚烷基二胺及其盐
公开(公告)号：US3969512A
公开(公告)日：1976-07-13
申请号：US548366
申请日：1975-02-10
申请人： Herbert Koppe , Helmut Stahle , Werner Kummer , Gojko Muacevic , Werner Traunecker
发明人： Herbert Koppe , Helmut Stahle , Werner Kummer , Gojko Muacevic , Werner Traunecker
IPC分类号： C07C275/24 , C07C275/34 , A61K31/135 , C07C93/06
CPC分类号： C07C275/34 , C07C275/24
摘要： Compounds of the formula ##EQU1## wherein R.sub.1 is allyl, allyloxy or chlorine, R.sub.2 is hydrogen or methyl,R.sub.3 is hydrogen, alkyl of 1 to 5 carbon atoms or benzyl, andn is an integer from 2 to 6, inclusive,Provided, however, that when R.sub.1 is allyl or allyloxy, R.sub.2 is hydrogen; and their non-toxic, pharmacologically acceptable acid addition salts; the compounds as well as their salts are useful as .beta.-adrenergic blocking agents and hypotensives.
摘要翻译：式-OCH2-CHOH-CH2-N-（CH2）nN-CH2 || R3R3 -CHOH-CH2-O-的化合物，其中R1是烯丙基，烯丙氧基或氯，R2是氢或甲基，R3是氢， 1至5个碳原子或苄基，N为2至6的整数，包括但不包括，当R1为烯丙基或烯丙氧基时，R2为氢; 及其无毒，药理学上可接受的酸加成盐; 化合物及其盐可用作β-肾上腺素能阻滞剂和低血糖剂。

35. 发明授权

US4409235A Substituted 7-(2,6-dibromo-4-methyl-phenyl)-2,3-dihydro-imidazo[1,2-a]imidazoles, compositions and use 失效
标题翻译：取代的7-（2,6-二溴-4-甲基 - 苯基）-2,3-二氢 - 咪唑并[1,2-a]咪唑，组合物和用途
公开(公告)号：US4409235A
公开(公告)日：1983-10-11
申请号：US404538
申请日：1982-08-02
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler
IPC分类号： A61K31/415 , A61P9/06 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of the formula ##STR1## wherein R is hydrogen or methyl, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.
摘要翻译：其中R为氢或甲基的式（IMAGE）化合物及其无毒的药学上可接受的酸加成盐。化合物及其盐可用作心动过缓。

36. 发明授权

US4263300A Substituted 2-phenylamino-1,3-tetrahydro-2-pyrimidines and salts thereof 失效
标题翻译：取代的2-苯基氨基-1,3-四氢-2-嘧啶及其盐
公开(公告)号：US4263300A
公开(公告)日：1981-04-21
申请号：US058164
申请日：1979-07-17
申请人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler
发明人： Helmut Stahle , Herbert Koppe , Werner Kummer , Walter Kobinger , Christian Lillie , Ludwig Pichler
IPC分类号： C07D239/10 , A61K31/34 , A61K31/38 , A61K31/505 , A61P9/00 , A61P9/08 , A61P9/10 , C07D239/14 , C07D405/12 , C07D409/12
CPC分类号： C07D239/14
摘要： This invention relates to 2-phenylamino-1,3-tetrahydro-2-pyrimidines of general formula ##STR1## wherein R is a radical selected from the group consisting of ##STR2##--CH.sub.2 --CH.dbd.CH.sub.2, --CH.sub.2 --CH.dbd.CH--CH.sub.3, and --CH.sub.2 --C(CH.sub.3).dbd.CH.sub.2,and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds, including the salts, are useful as bradycardiacs.
摘要翻译：本发明涉及通式为（I）的2-苯基氨基-1,3-四氢-2-嘧啶，其中R是选自下列基团的基团：-CH 2 -CH = CH 2，-CH 2 - CH = CH-CH 3和-CH 2 -C（CH 3）= CH 2，以及其无毒的药学上可接受的酸加成盐。包括盐的化合物可用作心动过缓。

37. 发明授权

US4031244A Pharmaceutical compositions containing a 1-(2,6-dimethyl-phenoxy)-2-amino-alkane and method of use 失效
标题翻译：含有1-（2,6-二甲基 - 苯氧基）-2-氨基 - 烷烃的药物组合物及其使用方法
公开(公告)号：US4031244A
公开(公告)日：1977-06-21
申请号：US653296
申请日：1976-01-29
申请人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Peter Danneberg
发明人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Peter Danneberg
IPC分类号： A61K31/135 , A61K31/55 , F41J11/02
CPC分类号： F41J11/02 , A61K31/135 , A61K31/55
摘要： Pharmaceutical compositions containing as an active ingredient a compound of the formula ##STR1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, and R.sub.1 is hydrogen or methyl, or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as anticonvulsives and antiarrhythmics.
摘要翻译：其中R为氢或1〜3个碳原子的烷基，R1为氢或甲基，或其无毒的药理学上可接受的酸加成盐作为活性成分含有下式化合物的药物组合物：以及使用其作为抗惊厥药和抗心律失常药的方法。

38. 发明授权

US4016202A 1-Phenoxy-2-hydroxy-3-alkynylamino-propanes and salts thereof 失效
公开(公告)号：US4016202A
公开(公告)日：1977-04-05
申请号：US609998
申请日：1975-09-03
申请人： Herbert Koppe , Werner Kummer , Helmut Stahle , Gojko Muacevic
发明人： Herbert Koppe , Werner Kummer , Helmut Stahle , Gojko Muacevic
IPC分类号： C07C275/34 , C07C93/06
CPC分类号： C07C275/34
摘要： Racemic and optically active compounds of the formula ##STR1## wherein R.sub.1 is hydrogen; halogen; nitro; alkyl of 1 to 5 carbon atoms; alkoxy of 1 to 4 carbon atoms; alkenyl of 2 to 5 carbon atoms; alkynyl of 2 to 5 carbon atoms; alkylamino of 1 to 5 carbon atoms; dialkylamino of 1 to 5 carbon atoms in each alkyl; alkoxyalkyl of 2 to 6 carbon atoms; alkylamino-alkyl of 2 to 6 carbon atoms; dialkylaminoalkyl of 3 to 12 carbon atoms; --(CH.sub.2).sub.x --NH.sub.2, --(CH.sub.2).sub.x -- OH, all where x is an integer from 0 to 3; --COOH; --COOR.sub.6, where R.sub.6 is alkyl of 1 to 4 carbon atoms; alkynyloxy of 3 to 6 carbon atoms; alkenyloxy of 3 to 6 carbon atoms; --CO--R.sub.9, --OCO--R.sub.9, --NH--CO--R.sub.9, all where R.sub.9 is alkyl of 1 to 6 carbon atoms, phenylalkyl of 7 to 10 carbon atoms or phenyl; cycloalkyl of 3 to 7 carbon atoms; --Q--CO--NR.sub.7 R.sub.8, where Q is a single bond, oxygen, --NH--, -- CH.sub.2 -- or --CH.sub.2 --NH--, and R.sub.7 and R.sub.8 are hydrogen, lower alkyl or, taken together with the nitrogen, pyrrolidino, piperidino or morpholino; phenyl; phenyl substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro, cyano and carboxyl; phenoxy; or phenoxy substituted with a substituent selected from the group consisting of halogen, lower alkyl, lower alkoxy, nitro, cyano and carboxyl;R.sub.2 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, alkanoyl of 2 to 4 carbon atoms, alkenyl of 2 to 4 carbon atoms, amino, nitro or, together with R.sub.1, 3,4-methylenedioxy;R.sub.3 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or, together with R.sub.2 in the ortho-position, --CH=CH--CH=CH-- or --(CH.sub.2)n--, where n is an integer from 3 to 5;R.sub.4 is hyddrogen or alkyl of 1 to 3 carbon atoms; andR.sub.5 is alkyl of 1 to 3 carbon atoms or, together with R.sub.4, --(CH.sub.2).sub.p -- where p is an integer from 4 to 6; and physiologically compatible acid addition salts thereof. The compounds as well as their salts are useful as adrenolytics and hypotensives.

39. 发明授权

US3975539A Pharmaceutical compositions containing an N,N-bis-(3-phenoxy-2-hydroxy-propyl)-alkylenediamine and method of use 失效
标题翻译：含有N，N-双 - （3-苯氧基-2-羟基 - 丙基） - 亚烷基二胺的药物组合物及其使用方法
公开(公告)号：US3975539A
公开(公告)日：1976-08-17
申请号：US568798
申请日：1975-04-16
申请人： Herbert Koppe , Helmut Stahle , Werner Kummer , Gojko Muacevic , Werner Traunecker
发明人： Herbert Koppe , Helmut Stahle , Werner Kummer , Gojko Muacevic , Werner Traunecker
IPC分类号： C07C275/24 , A61K31/275
CPC分类号： C07C275/24
摘要： Pharmaceutical compositions containing as an active ingredient a compound of the formula ##EQU1## wherein R.sub.1 is --(CH.sub.2).sub.x --CN, where x is 0,1,2 or 3,R.sub.2 is hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 5 carbon atoms, alkenyl of 2 to 5 carbon atoms or alkenyloxy of 2 to 5 carbon atoms;R.sub.3 is hydrogen, halogen, alkyl of 1 to 5 carbon atoms or alkoxy of 1 to 5 carbon atoms;R.sub.2 and R.sub.3, together with each other and the carbon atoms to which they are attached, form a saturated or unsaturated carbocyclic ring of up to 6 carbon atoms;R.sub.4 is hydrogen, alkyl of 1 to 5 carbon atoms or aralkyl; andn is an integer from 1 to 10, inclusive; or a non-toxic, pharmacologically acceptable acid addition salt thereof; and a method of using the same as .beta.-adrenergic receptor blockers and hypotensives.
摘要翻译：含有式-OCH 2 -CHOH-CH 2 -N（CH 2）n - | R N-CH 2 -CHOH-CH 2 -O-R 4的化合物作为活性成分的药物组合物，其中R1为 - （CH2）x-CN 其中x为0,1,2或3，R2为氢，卤素，1至5个碳原子的烷基，1至5个碳原子的烷氧基，2至5个碳原子的链烯基或2至5个碳原子的链烯氧基; R3是氢，卤素，1至5个碳原子的烷基或1至5个碳原子的烷氧基; R2和R3彼此连接并与它们相连的碳原子形成最多6个碳原子的饱和或不饱和碳环; R4是氢，1至5个碳原子的烷基或芳烷基; N是1到10的整数，包含; 或非毒性，药理学上可接受的酸添加盐; 以及使用它们作为β-受体阻断剂阻断剂和HYPTENSIVES的方法。

40. 发明授权

US3954872A 1-(2',6'-Dimethyl-phenoxy)-2-amino-alkanes and salts thereof 失效
标题翻译： 1-（2 {40,6（40-二甲基 - 苯氧基）-2-氨基 - 烷烃及其盐
公开(公告)号：US3954872A
公开(公告)日：1976-05-04
申请号：US511063
申请日：1974-10-01
申请人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Peter Danneberg
发明人： Herbert Koppe , Karl Zeile , Werner Kummer , Helmut Stahle , Peter Danneberg
IPC分类号： A61K31/135 , F41J11/02 , C07C93/06
CPC分类号： F41J11/02 , A61K31/135 , Y10S514/821
摘要： Compounds of the formula ##EQU1## wherein R is hydrogen or alkyl of 1 to 3 carbon atoms, andR.sub.1 is hydrogen or methyl,And non-toxic, pharmacologically acceptable acid addition salts thereof; the compounds as well as their salts are useful as anticonvulsives and antiarrhythmics in warmblooded animals.

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